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Claims for Patent: 8,293,794

Claims for Patent: 8,293,794

Title:

Methods and compositions for the treatment of CNS-related conditions

Abstract:

The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.

1. A pharmaceutical composition comprising: (a) 5 to 40 mg memantine or a pharmaceutically acceptable salt thereof provided in an extended release dosage form, wherein said
extended release memantine or pharmaceutically acceptable salt thereof provides a change in plasma concentration as a function of time (dC/dT) in a defined time period of 0 to 6 hours after administration, as measured in a single-dose human PK study,
that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine during said defined time period; and (b) a therapeutically effective amount of an ACheI or a pharmaceutically acceptable salt thereof
selected from the group consisting of donepezil, rivastigmine and galantamine.

2. A pharmaceutical composition of claim 1, wherein the ACheI is donepezil.

3. The composition of claim 1 wherein the concentration profile is further characterized by a maximum memantine plasma concentration to mean memantine plasma concentration ratio (Cmax/Cmean) of about 2.5 to 2 at 1 hour to at least 6 hours after
administration.

4. The composition of claim 1, wherein at least 98% of the memantine is in an extended release form.

5. The composition of claim 1, wherein the composition is a capsule and wherein the memantine, or pharmaceutically acceptable salt thereof, is formulated as pellets.

12. The composition of claim 1, wherein the ACheI is donepezil or a pharmaceutically acceptable salt thereof.

13. The composition of claim 12 wherein the donepezil or pharmaceutically acceptable salt thereof is in an immediate release form.

14. The composition of claim 1, wherein said extended release memantine or pharmaceutically acceptable salt thereof has an in vitro dissolution of less than 30% in one hour, less than 40% in two hours and greater than 40% in six hours as
measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37.+-.0.5.degree. C. with water as a dissolution medium.

15. A pharmaceutical composition comprising: (a) 5 to 40 mg memantine or a pharmaceutically acceptable salt thereof provided in an extended release dosage form, wherein said extended release memantine or pharmaceutically acceptable salt thereof
provides a change in plasma concentration as a function of time (dC/dT) that is less than about 50% of the dC/dT provided by the same quantity of an immediate release form of memantine during said defined time period, wherein the dC/dT is measured in a
single dose human PK study between the time period of 0 to Tmax of the immediate release form of memantine; and (b) a therapeutically effective amount of an ACheI or a pharmaceutically acceptable salt thereof selected from the group consisting of
donepezil, rivastigrnine and galantamine.

16. A pharmaceutical composition of claim 15, wherein the ACheI is donepezil.

17. The composition of claim 15, wherein the concentration profile is further characterized by a maximum memantine plasma concentration to mean memantine plasma concentration ratio (Cmax/Cmean) of about 2.5 to 2 at 1 hour to at least 6 hours
after administration.

18. The composition of claim 15, wherein at least 98% of the memantine is in an extended release form.

19. The composition of claim 15, wherein the composition is a capsule and wherein the memantine, or pharmaceutically acceptable salt thereof, is formulated as pellets.

26. The composition of claim 15, wherein the ACheI is donepezil or a pharmaceutically acceptable salt thereof.

27. The composition of claim 26, wherein the donepezil or pharmaceutically acceptable salt thereof is in an immediate release form.

28. The composition of claim 15, wherein said extended release memantine or pharmaceutically acceptable salt thereof has an in vitro dissolution of less than 30% in one hour, less than 40% in two hours and greater than 40% in six hours as
measured using a USP type 2 (paddle) dissolution system at 50 rpm, at a temperature of 37.+-.0.5.degree. C. with water as a dissolution medium.

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